LC-K2CAin-1

Chemical Structure : LC-K2CAin-1

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货号: PC-25380Not For Human Use, Lab Use Only.

LC-K2CAin-1 is a potent, highly selective CDK2-Cyclin A2 protein-protein interaction (PPI) inhibitor with IC50 of 59.57 nM in HTRF assays.

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生物&药学活性

LC-K2CAin-1 is a potent, highly selective CDK2-Cyclin A2 protein-protein interaction (PPI) inhibitor with IC50 of 59.57 nM in HTRF assays.
LC-K2CAin-1 shows no significantly affecting the interactions of CDK2 with Cyclin E1, CDK1 with Cyclin B1, CDK9 with Cyclin T1, or those of CDK4 and CDK6 with Cyclin D3.
LC-K2CAin-1 binds to and stabilizes the A-loop, inducing conformational changes of A-loop and α-C-Helix, which are likely responsible for the disruption of the CDK2–Cyclin A2 interaction.
LC-K2CAin-1 suppresses the proliferation of melanoma cells (A875cell, IC50=3.96 uM), and trigger apoptosis and induce G2/M phase arrest, but markedly less effective in CDK2-low VMM5A cells (IC50 > 14 µM).

物理化学性质&存储条件

分子量	525.57
分子式	C23H29F2N5O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(2,6-difluoro-3-(tetrahydro-2H-pyran-4-yl)benzamido)-N-(1-(ethylsulfonyl)piperidin-4-yl)-1H-pyrazole-3-carboxamide

参考文献

1. Sun G, et al. Angew Chem Int Ed Engl. 2025 Aug 19:e202513542.

LC-K2CAin-1

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物理化学性质&存储条件

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LC-K2CAin-1

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